Entecavir USP Tšilafalo B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir USP Tšilafalo B;Aids098045;Aids-098045;Etv;Enticavir;EntikaweiPian;
Entecavir (SQ 34676;BMS 200475) ke HBV Inhibitor e khethang le e sebetsang hantle.Ka liseleng tsa HepG2 boleng ba EC50 ke 3.75 nM.Litlhare tsa morao-rao tse thibelang lefu la sebete la mofuta oa B le li-anti-AIDS tsa pele.
Entecavir phello
Sehlahisoa sena ke guanine nucleoside analog, e nang le phello e thibelang kokoana-hloko ea hepatitis B (HBV) polymerase.E ka ba phosphorylated ho triphosphate e sebetsang, 'me halofo ea bophelo ba triphosphate ka seleng ke lihora tse 15.Ka ho hlōlisana le HBV polymerase's natural substrate deoxyguanosine triphosphate, entecavir triphosphate e ka thibela mesebetsi eohle e meraro ea kokoana-hloko ea polymerase (reverse transcriptase): (1) HBV polymerase initiation;(2) pregenomic mRNA Ho thehoa ha khoele e mpe ea reverse transcription;(3) Tšimoloho ea khoele e ntle ea HBV DNA.The inhibitory constant (Ki) ea entecavir triphosphate ho HBV DNA polymerase ke 0.0012μM.Entecavir triphosphate e na le phello e fokolang ea inhibitory ho sele α, β, δ DNA polymerase le mitochondrial γ DNA polymerase, e nang le Ki ea bohlokoa ea 18 ho 160 μM.
| Hlalosa | Entecavir (SQ 34676;BMS 200475) ke HBV Inhibitor e khethang ebile e sebetsa hantle.Ka har'a lisele tsa HepG2 boleng ba EC50 ke 3.75 nM. |
| Tse amananglihlopha | tsela ea pontšo >> Anti-infective >> HBV Research libaka >> Tšoaetso |
| Sepheo | EC50: 3.75 nM (anti-HBV, HepG2 cell)[2] |
| In vitrolithuto | EC50 ea BMS-200475 ho ea ho HBV ke 3.75 nM.E kenyelelitsoe ho li-primers tsa protheine ea HBV, ebe mohato oa ho qala oa reverse transcriptase oa thibeloa.Ts'ebetso ea antiviral ea BMS-200475 e tlase haholo ho feta livaerase tse ling tsa RNA le DNA [1].Ha ho bapisoa le li-analogues tse ling tsa deoxyguanosine (penciclovir, ganciclovir, lobucavir le acyclovir) kapa lamivudine, entecavir e ka 'na ea e-ba phosphorylated ho metabolite ea eona e sebetsang.Bophelo ba halofo ea intracellular ea Entecavir ke lihora tsa 15 [2]. |
| Ka vivolipatlisiso | BMS-200475 e tšoaroa ka molomo letsatsi le leng le le leng ka tekanyo e tsoang ho 0.02 ho 0.5 mg / kg boima ba 'mele bakeng sa 1 ho likhoeli tsa 3, e ka fokotsang ka katleho boemo ba woodchuck hepatitis virus (WHV) viremia ka mapolanka a nang le tšoaetso e sa foleng [3]. |
| Seleteko | BMS 200475 e hlophisitsoe ka phosphate buffered saline (PBS) mme e hlapolotsoe ka mokhoa o loketseng o nang le serum ea 2% ea fetal bovine.Lisele tsa HepG2 2.2.15 li ile tsa jaloa holim'a poleiti e koahetsoeng ka collagen ea 12-liliba ea Biocoat ka bongata ba lisele tse 5 × 10 5 selibeng ka seng, 'me e bolokiloe sebakeng se kopaneng bakeng sa matsatsi a 2 ho isa ho a 3, ebe e koahetsoe ka 1 ml ea BMS 200475. mahareng .Tlhahlobo ea HBV e entsoe ka letsatsi la 10 [1]. |
| Litšupiso | [1].Innaimo SF, le ba bang.Ho khetholla BMS-200475 e le inhibitor e matla le e khethollang ea kokoana-hloko ea hepatitis B.Antimicrob Agents Chemother.1997 Jul;41(7):1444-9.[2].Rivkin A, le ba bang.Tlhahlobo ea entecavir ha ho phekoloa tšoaetso e sa foleng ea lefu la sebete la mofuta oa B.Curr Med Res Opin.2005 Nov;21(11):1845-57.[3].Genovesi EV, et al.Katleho ea carbocyclic 2'-deoxyguanosine nucleoside BMS-200475 ka mohlala oa woodchuck oa tšoaetso ea kokoana-hloko ea hepatitis B.Antimicrob Agents Chemother.1998 Dec;42(12):3209-18. |
Lintho tsa 'mele le tsa lik'hemik'hale tsa Entecavir
| Botenya | 1.8±0.1 g/cm3 |
| Ntho e belang | 734.2ºC ho 760 mmHg |
| Sebaka se qhibilihang | 249-252ºC |
| Mokhoa oa limolek'hule | C12H15N5O3 |
| Boima ba molek'hule | 277.279 |
| flash point | 397.9ºC |
| Boleng bo nepahetseng | 277.117493 |
| PSA | 130.05000 |
| LogP | -0.96 |
| Litšobotsi tsa ponahalo | Phofo ea kristale e tšoeu ho ea ho e tšoeu / mosehla |
| Lenane la refractive | 1.837 |
| Maemo a polokelo | -20°C Sehatsetsi |
Mekhoa ea Entecavir
| Melao ea meetlo | 2933990099 |
| Chinese Overview | 2933990099. Metsoako e meng ea heterocyclic e nang le li-heteroatom tsa nitrogen feela.Sekhahla sa lekhetho la boleng bo eketsehileng: 17.0%.Sekhahla sa phokotso ea lekhetho: 13.0%.Maemo a taolo: Ha ho letho.Litefiso tsa naha tse ratoang haholo: 6.5%.Litefiso tse akaretsang: 20.0% |
| Lintlha tsa phatlalatso | Lebitso la sehlahisoa, dikahare tsa motsoako, tšebeliso, hexamethylene chloride, ka kopo bonts'a ponahalo, 6-caprolactam, ka kopo bonts'a ponahalo, letsatsi la ho saena. |
| Kakaretso | 2933990090. metsoako ea heterocyclic e nang le nitrogen hetero-athomo feela.VAT:17.0%.Sekhahla sa phokotso ea lekhetho: 13.0%..Litefiso tsa MFN: 6.5%.Litefiso tse akaretsang: 20.0% |
Tlhahisoleseling e 'Ngoe:
Qu Qiang (PhD ho pharmacology ea bongaka, Lefapha la Pharmacy, Sepetlele sa Xiangya, Central South University) le Wang Ruoguang (Ngaka ea Bongaka, postdoctoral in biology, Changsha Ruoguang Medical Research Center) le bona ba ngotse hore: ka mokhoa oa entecavir, entecavir e ka nkoa. lilemo tse 'maloa kapa esita le lilemo tse 10.Ho feta lilemo.'Me e ka sebelisoa ke bakhachane, ho bontša tšireletso e ntle.
Ho latela mekhoa ena e tsebahalang ea limolek'hule tsa pharmacological, Entecavir e ka 'na ea e-ba le phello e pharaletseng ea antiviral, eseng feela e sebetsang khahlanong le HBV.
Hape re atisa ho sebelisa Entecavir ho phekola tšoaetso ea kokoana-hloko ea ho hema tleliniking, 'me phello e tsoteha.
Hajoale, tlhahlobong ea morao-rao ea bakuli ba fetang 500 ba COVID19 ba Hubei (sebaka), ke motho a le mong feela ea nkileng entecavir.Nako ea lengolo la ngaka e ne e le mathoasong a January, 'me joale moriana o emisitsoe.
Ha a ntse a ts'ehetsa basebetsi ba tsa bongaka Hubei, lingaka tse ling tsa mantlha, kapa lihlopha tse kotsing e kholo, tse sebelisang Entecavir ho thibela COVID19, ha ho na taba ea ts'oaetso.Batho bao ho belaelloang hore ba nka entecavir, ha ho motho ea tsoetseng pele ho fumanoa a e-na le COVID19.
Litaba tsa Patent:
Haholo-holo ho na le lits'ebetso tse peli, ts'ebetso ea 06 le ts'ebetso ea 89.Ho felloa ke nako ha tokelo ea molao bakeng sa ts'ebetso ea 06 ho sa le pele haholo (e felloa ke nako ka 2023)!Le hoja litšenyehelo tsa ts'ebetso li le tlaase, boleng bo batla bo le botle, 'me basebetsi ba ka ba le keletso e matla, ea botho: Bakeng sa limela tsa lik'hemik'hale, sebelisa mokhoa oa 06 hore u se ke ua ikhohomosa haholo;bakeng sa lik'hamphani tsa meriana, u se ke ua nka fluke 'me u se ke ua ba kotsi haholo .
Ka 2014, Chia Tai Tianqing e fihletse thekiso ea selemo le selemo ea li-yuan tse limilione tse likete tse 10 ka ho itšetleha ka lithethefatsi tse tloaelehileng tse kang entecavir, eo entecavir e neng e le 20%.
Kaha entecavir e ile ea amoheloa bakeng sa ho kenngoa ka 2005, lik'hamphani tse fetang 100 tsa malapeng tsa meriana li kentse kopo ea ho ngolisoa ha sehlahisoa;har'a bona, lik'hamphani tse amohelehang tsa tlhahiso li kenyelletsa Jiangsu Zhengda Tianqing Pharmaceutical (e etsisang pele), Hainan Zhonghe Pharmaceutical, le Fujian Guangxi Pharmaceutical Co., Ltd. Shengtang Pharmaceutical, Jiangxi Qingfeng Pharmaceutical, Suzhou Dawnrays Pharmaceutical, Shanghai Pharmaceutical Pharmaceutical, Quingchuing Pharmaceutical, Shanghai. Lukang, Zhejiang Huasheng Biopharmaceutical, Changzhi Sanbao Biochemical.
Pharmaceutical, Anhui Baker Biopharmaceutical, Hunan Concord Pharmaceutical Industry, Beijing Xiehe Pharmaceutical Factory, Beijing Baiao Pharmaceutical, Xinlitai Pharmaceutical, Dongyangguang, joalo-joalo;ho tloha ka letsatsi la konteraka, sehlahisoa sena se kene maemong a mefuta e tsebahalang e phatlalalitsoeng ho tloha ka 2007.
JIN DUN Medical o na leHo tšoaneleha ha ISO mme e kopana le litekanyetso tsa tlhahiso ea GMP, e hirileng litsebi tsa ka hare ho naha le tsa kantle ho naha tse nang le boiphihlelo bo bongata ho tataisa R&D ea k'hamphani.
THEKNOL OGY MELEMO
● High Pressure Catalytic Hydrogenation .Khatello e Phahameng ea Hydrogenolysis Reaction .Mehato ea Cryogenic (<-78%C)
● Monko o monate oa Heterocyclic Synthesis
● Karabelo ea ho Rulahanya bocha
●Chiral Resolution
●Heck, Suzuki,Negishi,Sonogashira .Giignard Reaction
Thepa
Lab ea rona e na le lisebelisoa tse fapaneng tsa liteko le liteko, joalo ka: NMR (Bruker 400M), HPLC, chiral-HPLC, LC-MS, LC-MS/MS (API 4000), IR, UV, GC, GC-MS, Chromatography, Microwave Synthesizer, Parallel Synthesizer, Differential Scanning Calorimeter (DSC), Electron microscope...
Sehlopha sa R&D
Jindun Medical e na le sehlopha sa basebetsi ba profeshenale ba R&D, 'me e sebelisa litsebi tse ngata tsa lapeng le kantle ho naha ho tataisa R&D, ho etsa hore pokello ea rona e nepahale le ho sebetsa hantle.
Re thusitse lik'hamphani tse ngata tse phahameng tsa malapeng tsa meriana, tse kangHansoh, Hengrui le HEC Pharm.Mona re tla bontša karolo ea bona.
Customization Case One:
Cas No.: 110351-94-5
Taba ea Bobeli ea Tloaelo:
Cas No.: 144848-24-8
Taba ea Boraro ea Tloaelo:
Cas No.: 200636-54-0
1.Iketsetse Li-Intermediate tse Ncha kapa li-API.Joalo ka ho arolelana linyeoe tse kaholimo, bareki ba na le litlhoko tsa li-Intermediates kapa li-API, 'me ha ba khone ho fumana lihlahisoa tse hlokahalang' marakeng, joale re ka thusa ho Customize.
2.Ntlafatso ea Ts'ebetso ea Lihlahisoa tsa Khale.Sehlopha sa rona se tla thusa ho ntlafatsa le ho ntlafatsa tlhahiso e joalo eo tsela ea eona ea ho arabela e leng ea khale, litšenyehelo tsa tlhahiso li phahame, 'me katleho e tlaase.Re ka fana ka litokomane tse felletseng bakeng sa phetisetso ea theknoloji le ntlafatso ea ts'ebetso, re thusa moreki bakeng sa tlhahiso e sebetsang hantle.
Ho tloha ho sepheo sa lithethefatsi ho isa ho INDs, JIN DUN Medical e u falitharollo tsa motho ka mong tsa R&D.
JIN DUN Medical e tsitlallela ho theha sehlopha se nang le litoro, ho etsa lihlahisoa tse nang le seriti, tse hlokolosi, tse thata, le ho tsoa bohle ho ba molekane ea tšepahalang le motsoalle oa bareki!
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